Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T00140 | Target Info | |||
| Target Name | Arachidonate 5-lipoxygenase (5-LOX) | ||||
| Synonyms |
LOG5; 5-lipoxygenase; 5-LO
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| Target Type | Successful Target | ||||
| Gene Name | ALOX5 | ||||
| Biochemical Class | Oxygenase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| Co-Target Name | Platelet-activating factor receptor (PTAFR) | Successful Target | ||||
| UniProt ID | PTAFR_HUMAN | |||||
| Gene Name | PTAFR | |||||
| Synonyms |
PTAFR; PAF-R
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| Representative Drug(s) | CMI-392 | Drug Info | IC50 = 10 nM | [1] | ||
| Co-Target Name | Prostaglandin G/H synthase 1 (COX-1) | Successful Target | ||||
| UniProt ID | PGH1_HUMAN | |||||
| Gene Name | PTGS1 | |||||
| Synonyms |
Prostaglandin-endoperoxide synthase 1; Prostaglandin H2 synthase 1; PHS 1; PGHS-1; PGH synthase 1; Cyclooxygenase-1; COX1; COX-1
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| Representative Drug(s) | Darbufelone | Drug Info | IC50 = 600 nM | [2] | ||
| Co-Target Name | Leukotriene A-4 hydrolase (LTA4H) | Successful Target | ||||
| UniProt ID | LKHA4_HUMAN | |||||
| Gene Name | LTA4H | |||||
| Synonyms |
Leukotriene A4 hydrolase; Leukotriene A(4)Leukotriene A-4 hydrolase hydrolase; Leukotriene A(4) hydrolase; LTA4; LTA-H; LTA-4hydrolase; LTA-4 hydrolase
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| Representative Drug(s) | Zileuton | Drug Info | IC50 = 850 nM | [3] | ||
| Co-Target Name | Indoleamine 2,3-dioxygenase 1 (IDO1) | Successful Target | ||||
| UniProt ID | I23O1_HUMAN | |||||
| Gene Name | IDO1 | |||||
| Synonyms |
Indoleamine-pyrrole 2,3-dioxygenase; INDO; IDO-1; IDO
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| Representative Drug(s) | Avastin+/-Tarceva | Drug Info | IC50 = 1000 nM | [4] | ||
| Co-Target Name | Leukotriene B4 receptor 1 (LTB4R) | Clinical trial Target | ||||
| UniProt ID | LT4R1_HUMAN | |||||
| Gene Name | LTB4R | |||||
| Synonyms |
P2Y7; P2Y purinoceptor 7; P2RY7; Leukotriene B(4) receptor BLT1; LTB4-R1; LTB4-R 1; LTB4-R; GPR16; G-protein coupled receptor 16; Chemoattractant receptor-like 1; CMKRL1; BLTR; BLT1; BLT
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| Representative Drug(s) | Zileuton | Drug Info | IC50 = 420 nM | [5] | ||
| Co-Target Name | Soluble epoxide hydrolase (EPHX2) | Clinical trial Target | ||||
| UniProt ID | HYES_HUMAN | |||||
| Gene Name | EPHX2 | |||||
| Synonyms |
Bifunctional epoxide hydrolase 2
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| Representative Drug(s) | Zileuton | Drug Info | IC50 = 591 nM | [6] | ||
| Co-Target Name | Prostaglandin E synthase (PTGES) | Clinical trial Target | ||||
| UniProt ID | PTGES_HUMAN | |||||
| Gene Name | PTGES | |||||
| Synonyms |
p53-induced gene 12 protein; PIG12; PGES; PGE synthase; P53-induced apoptosis protein 12; Microsomal prostaglandin E synthase 1; Microsomal glutathione S-transferase 1-like 1; MPGES1; MPGES-1; MGST1L1; MGST1-L1
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| Representative Drug(s) | Zileuton | Drug Info | IC50 = 600 nM | [7] | ||
| Co-Target Name | Arachidonate 15-lipoxygenase (15-LOX) | Patented-recorded Target | ||||
| UniProt ID | LOX15_HUMAN | |||||
| Gene Name | ALOX15 | |||||
| Synonyms |
LOG15; Arachidonate omega-6 lipoxygenase; Arachidonate 12-lipoxygenase, leukocyte-type; 15-Lipoxygenase; 15-LOX-1; 12/15-lipoxygenase; 12-LOX
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| Representative Drug(s) | Zileuton | Drug Info | IC50 = 400 nM | [8] | ||
| Co-Target Name | Arachidonate 5-lipoxygenase activating protein (FLAP) | Discontinued Target | ||||
| UniProt ID | AL5AP_HUMAN | |||||
| Gene Name | ALOX5AP | |||||
| Synonyms |
MK-886-binding protein; FLAP; ALOX5AP
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| Representative Drug(s) | Zileuton | Drug Info | IC50 = 580 nM | [9] | ||
| References | Top | ||||
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| REF 1 | (+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-3... J Med Chem. 1998 May 21;41(11):1970-9. | ||||
| REF 2 | Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series. J Med Chem. 1999 Apr 8;42(7):1151-60. | ||||
| REF 3 | Structure-activity relationship studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase. J Med Chem. 2000 Feb 24;43(4):721-35. | ||||
| REF 4 | Indoleamine 2,3-dioxygenase is the anticancer target for a novel series of potent naphthoquinone-based inhibitors. J Med Chem. 2008 Mar 27;51(6):1706-18. | ||||
| REF 5 | Structure-activity relationships of (E)-3-(1,4-benzoquinonyl)-2-[(3-pyridyl)-alkyl]-2-propenoic acid derivatives that inhibit both 5-lipoxygenase and thromboxane A2 synthetase. J Med Chem. 1996 Aug 2;39(16):3148-57. | ||||
| REF 6 | Synthesis and structure-activity relationship studies of novel dual inhibitors of soluble epoxide hydrolase and 5-lipoxygenase. J Med Chem. 2013 Feb 28;56(4):1777-81. | ||||
| REF 7 | Discovery of a benzenesulfonamide-based dual inhibitor of microsomal prostaglandin E. Eur J Med Chem. 2018 Aug 5;156:815-30. | ||||
| REF 8 | Easy and rapid preparation of benzoylhydrazides and their diazene derivatives as inhibitors of 15-lipoxygenase. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1649-53. | ||||
| REF 9 | 4,5-Diarylisoxazol-3-carboxylic acids: A new class of leukotriene biosynthesis inhibitors potentially targeting 5-lipoxygenase-activating protein (FLAP). Eur J Med Chem. 2016 May 4;113:1-10. | ||||
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